Structural Modelling of the Human Drug-Metabolizing Cytochromes P450

Author(s): David F.V. Lewis, Yuko Ito, Peter S. Goldfarb.

Journal Name: Current Medicinal Chemistry

Volume 13 , Issue 22 , 2006


The structural and functional aspects of cytochrome P450 (CYP) enzymes are reviewed in the light of current developments in X-ray crystallography and other physical evidence, together with recent findings on the regulation of, and polymorphisms in, the human drug-metabolizing CYPs. It is emphasized that the crystal structures of eukaryotic CYPs are particuarly useful for constructing homology models of the human enzymes associated with drug metabolism, and that these models can aid in the high-throughput screening of novel compounds destined for human exposure.

Keywords: Cytochromes P450 (CYPs), drug metabolism, enzyme structure and function

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Article Details

Year: 2006
Page: [2645 - 2652]
Pages: 8
DOI: 10.2174/092986706778201567
Price: $58

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